Transmucosal delivery of cannabinoids

a cannabinoid and transmucosal technology, applied in the direction of biocide, plant/algae/fungi/lichens ingredients, bandages, etc., can solve the problems of rapid reduction of the concentration level of the chemical in the bloodstream, rapid metabolization in the body, etc., to limit the bioavailability of the chemical, high lipophilicity, and strong binding

Inactive Publication Date: 2006-11-16
UNIVERSITY OF MISSISSIPPI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012] Although the chemical and physical properties of the cannabinoids have limited their bioavailability, it has been discovered that their bioavailability can be very effective via the described transmucosal delivery system in this invention. Polyethylene glycol 400 has been reported in the scientific literature to act as an absorption enhancer of the skin. It (and other solubilizers) may also serve as an absorption enhancer of cannabinoids for the mucosa, in addition to functioning as a solubilizer for the cannabinoid for the hot-melt extrusion, hot-melt molding and admixing processes or solvent cast techniques. The primary active ingredient of cannabis is THC, which is effective at relatively low doses. Due to its high lipophilicity, THC exhibits a strong tendency to bind to tissue and protein—thus making the discussed transmucosal applications plausible routes of delivery. Furthermore, mHC is rapidly metabolized in the body, such that concentration levels of the chemical in the bloodstream decreases rapidly if administered through inhalation methods. A transmucosal application, in contrast to inhalation methods allows for smaller dosages of THC to be administered over an extended period of time, thereby allowing the concentration levels of the drug in the blood stream to remain relatively constant. In addition, and of utmost importance, the smaller doses of the transmucosal route reduce the potential for abuse.
[0013] The present invention comprises a transmucosal device, such as, but not limited to, an intra-oral, labial or buccal patch, strip, covering, or related assembly of materials to deliver THC or other cannabinoids in a predetermined period of time. One purpose of the structure or method is to allow for controlled delivery of the active chemicals, such that plasma levels of the chemicals may be controlled in a safe, convenient and effective manner for the patient.

Problems solved by technology

Furthermore, mHC is rapidly metabolized in the body, such that concentration levels of the chemical in the bloodstream decreases rapidly if administered through inhalation methods.

Method used

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  • Transmucosal delivery of cannabinoids

Examples

Experimental program
Comparison scheme
Effect test

example # 1

EXAMPLE #1

Transmucosal Device for THC Delivery via the Oral Mucosa

[0043]

InnerOuterIngredientsmatrix (%)backing layerHydroxypropylcellulose75.9037.00(Klucel ®-EF)Polycarbophil (Noveon ® AA-1)5.00Polyethylene glycol 4008.00Tartaric Acid3.00BHT0.10Tetrahydrocannabinol (THC)8.00Ethyl cellulose60.00Eudragit ® E-1002.00Polyethylene glycol 33501.00

[0044] Example #1 above contains the solubilizer PEG 400, which may also function as a penetration enhancer. An additional example (Example #1a) may include the above formula with the bile salt penetration enhancer, sodium deoxycholate, at the 5% level.

example # 2

EXAMPLE #2, #3, #4

[0045]

Drug / Chemical (% w / w)#2#3#4Hydroxypropyl cellulose (Avg MW: 80,000)15.511.53.5Polyethylene Oxide (Avg MW: 200,000)80.480.480.4Vitamin E succinate0.10.10.1Tetrahydrocannabinol Hemiglutarate4816(THC Pro-drug)

[0046] Example #2-#4 were prepared via a solvent cast technique. The Tetrahydrocannabinol Hemiglutarrate (THC-HG) was dissolved in ethanol (10% w / w of THC-HG). The HPC and PEO were then admixed with the Vitamin E succinate via solvation. Then the THC-HG solution was slowly added to the polymeric dispersion. The resulting dispersion was added to a film forming mold and the solvent was evaporated off. The resulting transmucosal preparation was homogenously dispersed with the cannabinoid pro-drug.

[0047] Example #5 and #6 were prepared using hot-melt extrusion techniques. The formulas are listed below. The PEO, PVP and Vitamin E TPGS were dry blended in a V-blender. The THC and the THC-HS were solubilized in the PEG 400 and immediately sprayed into the dry ble...

examples # 5 & # 6

EXAMPLES #5 & #6

[0048]

Drug / Chemical (% w / w)#5#6Polyethylene Oxide (Avg MW: 1,000,000)68.068.0Polyvinylpyrrolidone (Kollidon)10.010.0Polyethylene glycol (PEG 400)11.011.0Vitamin E TPGS3.03.0Tetrahydrocannabinol (THC)8.0—Tetrahydrocannabinol Hemisuccinate—8.0(THC-HS)

[0049] Diffusion studies of the transmucosal preparation films in Examples #5 and #6 were performed using a PermeGear, Model V9, 9 Cell System. Modified Franz cells were employed using thinly-excised rabbit mucosa as the diffusion membrane. Diffusion media was a diffusion buffer system of Brij® 3.0% (pH=7.2) which was determined by previous testing. FIG. 1 illustrates the results of these studies. As can be seen by the illustration, the THC-HS exhibited a more immediate release with controlled diffusion for over 22 hours. Example #5 (THC) demonstrated a slower release with approximately 50% theoretical drug released at 22 hours. Both formulations have clinical applications for different therapeutic objectives.

[0050] It ha...

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Abstract

A method of transmucosally delivering a cannabinoid to a subject in need of such treatment comprising the steps of: administering to the subject a transmucosal preparation containing the cannabinoid wherein said transmucosal preparation is made by incorporating an effective amount of the cannabinoid via hot-melt extrusion technology, hot-melt molding, admixing or a solvent cast technique into a film matrix or a reservoir containing the cannabinoid, and attaching said transmucosal preparation to the mucosa of the subject.

Description

FIELD OF THE INVENTION [0001] This invention pertains to methods and products for the transmucosal administration of cannabinoids. In addition, this invention concerns a system for delivering effective dosages of cannabinoids to one's bloodstream. BACKGROUND OF THE INVENTION [0002] Products and methods for transdermally administering particular chemicals are known in the art. Several U.S. patents have issued for the transdermal application of chemicals, most recently for cannabis (Brooke, et al., U.S. Pat. No. 6,113,940). Other methods and products for transmucosally delivering chemicals are also known in the art. However, this invention expands the concept of transdermal delivery of cannabis and the transmucosal delivery of other chemicals. The physico-chemical properties of cannabinoids (low water solubility, questionable stability, poor bioavailability) have limited its oral bioavailability and bioavailability via other routes of absorption. Discoveries disclosed within this inve...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K36/88A61K31/353A61K9/70A61K9/00A61K47/10A61K47/12
CPCA61K9/006A61K9/127A61K9/1272A61K47/12A61K36/185A61K47/10A61K31/353
Inventor ELSOHLY, MAHMOUDREPKA, MICHAEL A.
Owner UNIVERSITY OF MISSISSIPPI
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